Riferimento:
Bioorg Med Chem. 2012 Dec 1;20(23):6877-84.
Autori:
Gardner CR, Cheung BB, Koach J, Black DS, Marshall GM, Kumar N.
Fonte:
Bioorg Med Chem. 2012 Dec 1;20(23):6877-84.
Anno:
2012
Azione:
2-aminobenzotiazolo è stato testato contro linee cellulari di neuroblastoma e di adenocarcinoma mammario, mostrando attività citotossica in aggiunta ad un basso dosaggio di acido 13-cis-retinoico.
Target:
2-Aminobenzotiazolo, Acido 13-cis-retinoico/neuroblastoma, adenocarcinoma mammario.
ABSTRACT
Indole-3-amides and dipeptides were produced from 2-aminobenzothiazoles using the PyBop peptide coupling reagent. These analogues were tested in anti-cancer cell viability assays against SH-SY5Y neuroblastoma and MDA-MB-231 breast adenocarcinoma cell lines, and were found to exhibit cytotoxic activities at concentrations ranging from 0.1 to 20μM. These compounds were also found to act additively with a low dosage of 13-cis-retinoic acid in neuroblastoma cells. Then, using neuroblastoma cells transfected to stably overexpress the RARβ(2) gene, a SAR was developed for the indole-3-amides. Real-time PCR was also used to demonstrate their RARβ(2) agonistic activity.
Sostanze: